AI Article Synopsis
- - Discovery of compound 19 as a strong CYP11B2 inhibitor that is selective over similar enzymes and has favorable pharmacokinetic characteristics in rat and rhesus models
- - Compound 19 has desirable physical properties, making it a promising lead in drug development
- - In a study with rhesus monkeys, compound 19 effectively lowers aldosterone levels in a dose-dependent manner, without affecting cortisol levels.
Article Abstract
Hit-to-lead efforts resulted in the discovery of compound 19, a potent CYP11B2 inhibitor that displays high selectivity vs related CYPs, good pharmacokinetic properties in rat and rhesus, and lead-like physical properties. In a rhesus pharmacodynamic model, compound 19 displays robust, dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4538427 | PMC |
| http://dx.doi.org/10.1021/acsmedchemlett.5b00048 | DOI Listing |
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